[The pharmacokinetics of 2-methyl-4-nitroimidazole-1-ethanol (isometronidazole) in man]

2 and 4 g isometronidazole, respectively, were administered to two groups of 6 healthy male volunteers (21-29 years, 62-93 kg). The unchanged compound and its nitro group containing metabolites were measured by HPLC and polarography. Isometronidazole was absorbed rapidly, distributed slowly into peripheral compartments and eliminated with half lives of about 12 h. It was not bound to plasma proteins. On an average 70% (2 g) and 80% (4 g), respectively, were excreted into urine within 48 h both unchanged and in form of at least two more polar and/or water soluble metabolites. Distribution and excretion of isometronidazole were not proportional to dose.